EA012607B1 - НОВЫЕ ГЕТЕРОЦИКЛИЧЕСКИЕ ИНГИБИТОРЫ NF-κB - Google Patents

НОВЫЕ ГЕТЕРОЦИКЛИЧЕСКИЕ ИНГИБИТОРЫ NF-κB Download PDF

Info

Publication number
EA012607B1
EA012607B1 EA200700441A EA200700441A EA012607B1 EA 012607 B1 EA012607 B1 EA 012607B1 EA 200700441 A EA200700441 A EA 200700441A EA 200700441 A EA200700441 A EA 200700441A EA 012607 B1 EA012607 B1 EA 012607B1
Authority
EA
Eurasian Patent Office
Prior art keywords
group
alkyl
phenyl
piperazin
thiazol
Prior art date
Application number
EA200700441A
Other languages
English (en)
Russian (ru)
Other versions
EA200700441A1 (ru
Inventor
Иоганн Лебан
Харальд Шмитт
Кристина Вольф
Стефано Пегораро
Андреас Вуцик
Original Assignee
4Сц Аг
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from EP04022363A external-priority patent/EP1637529A1/en
Application filed by 4Сц Аг filed Critical 4Сц Аг
Publication of EA200700441A1 publication Critical patent/EA200700441A1/ru
Publication of EA012607B1 publication Critical patent/EA012607B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/34—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D263/48—Nitrogen atoms not forming part of a nitro radical
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/10—Anti-acne agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular system
    • A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/08—Antiepileptics; Anticonvulsants
    • A61P25/12—Antiepileptics; Anticonvulsants for grand-mal
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/56—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Vascular Medicine (AREA)
  • Immunology (AREA)
  • Psychiatry (AREA)
  • Psychology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Virology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
EA200700441A 2004-09-20 2005-07-29 НОВЫЕ ГЕТЕРОЦИКЛИЧЕСКИЕ ИНГИБИТОРЫ NF-κB EA012607B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP04022363A EP1637529A1 (en) 2004-09-20 2004-09-20 Novel piperidin-4-yl-thiazole-carboxamide analogues as inhibitors of T-cell proliferation and uses thereof
US61279404P 2004-09-27 2004-09-27
PCT/EP2005/008261 WO2006032322A1 (en) 2004-09-20 2005-07-29 NOVEL HETEROCYCLIC NF-κB INHIBITORS

Publications (2)

Publication Number Publication Date
EA200700441A1 EA200700441A1 (ru) 2007-10-26
EA012607B1 true EA012607B1 (ru) 2009-10-30

Family

ID=43500491

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200700441A EA012607B1 (ru) 2004-09-20 2005-07-29 НОВЫЕ ГЕТЕРОЦИКЛИЧЕСКИЕ ИНГИБИТОРЫ NF-κB

Country Status (11)

Country Link
US (1) US8106048B2 (ja)
EP (1) EP1797084A1 (ja)
JP (1) JP2008513386A (ja)
CN (1) CN101031567B (ja)
AU (1) AU2005287692B2 (ja)
BR (1) BRPI0516958A (ja)
CA (1) CA2580725A1 (ja)
EA (1) EA012607B1 (ja)
MX (1) MX2007003115A (ja)
NZ (1) NZ553734A (ja)
WO (1) WO2006032322A1 (ja)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1637529A1 (en) 2004-09-20 2006-03-22 4Sc Ag Novel piperidin-4-yl-thiazole-carboxamide analogues as inhibitors of T-cell proliferation and uses thereof
EP1797084A1 (en) * 2004-09-20 2007-06-20 4Sc Ag NOVEL HETEROCYCLIC NF-kB INHIBITORS
US7601745B2 (en) * 2004-09-27 2009-10-13 4Sc Ag Heterocyclic NF-kB inhibitors
US20100267717A1 (en) * 2005-07-29 2010-10-21 4Sc Ag Novel Heterocyclic NF-kB Inhibitors
DE102005033103A1 (de) * 2005-07-15 2007-01-25 Bayer Healthcare Ag Heterocyclylamid-substituierte Thiazole, Pyrrole und Thiophene
TW200738701A (en) * 2005-07-26 2007-10-16 Du Pont Fungicidal carboxamides
KR20080031038A (ko) * 2005-07-29 2008-04-07 4에스체 악티엔게젤샤프트 신규의 헤테로환 ＮＦ-κＢ 억제제
EP1832586A1 (en) * 2006-03-10 2007-09-12 Oridis Biomed Forschungs- und Entwicklungs GmbH Thiazole-piperidine derivatives in treatment of diseases of liver and the pancreas
EP1834954A1 (en) * 2006-03-15 2007-09-19 4Sc Ag Thiazoles as NF-kB Inhibitors (proteasome inhibitors)
CN101405278A (zh) * 2006-03-15 2009-04-08 4Sc股份公司 新颖的杂环NF-κB抑制剂
BRPI0709595A2 (pt) * 2006-03-15 2011-07-19 4Sc Ag inibidores de nf-kapab heterocìclicos
US9090604B2 (en) 2006-07-27 2015-07-28 E I Du Pont De Nemours And Company Fungicidal azocyclic amides
WO2008013622A2 (en) * 2006-07-27 2008-01-31 E. I. Du Pont De Nemours And Company Fungicidal azocyclic amides
TW200819437A (en) * 2006-08-17 2008-05-01 Astrazeneca Ab Chemical compounds
TWI428091B (zh) 2007-10-23 2014-03-01 Du Pont 殺真菌劑混合物
EP2334669B1 (de) 2008-10-01 2015-12-23 Bayer Intellectual Property GmbH Heterocyclyl substituierte thiazole als pflanzenschutzmittel
SG11201401084TA (en) * 2011-09-30 2014-04-28 Kineta Inc Anti-viral compounds
AU2014249003A1 (en) 2013-03-13 2015-10-15 Forma Therapeutics, Inc. Novel compounds and compositions for inhibition of FASN
AU2014283378B2 (en) * 2013-06-18 2018-09-27 4Sc Ag 2,3-dihydrobenzofuran-5-yl compounds as DYRK kinase inhibitors
CN103432118B (zh) * 2013-08-30 2016-05-04 暨南大学 穿心莲内酯衍生物在制备预防和治疗神经退行性疾病药物中的应用
NZ722487A (en) * 2014-01-29 2022-04-29 Ucb Biopharma Sprl Heteroaryl amides as inhibitors of protein aggregation
WO2017122209A2 (en) * 2016-01-12 2017-07-20 Yeda Research And Development Co. Ltd. NF-kappaB INHIBITORS
TWI767148B (zh) 2018-10-10 2022-06-11 美商弗瑪治療公司 抑制脂肪酸合成酶(fasn)
US10793554B2 (en) 2018-10-29 2020-10-06 Forma Therapeutics, Inc. Solid forms of 4-(2-fluoro-4-(1-methyl-1H-benzo[d]imidazol-5-yl)benzoyl)piperazin-1-yl)(1-hydroxycyclopropyl)methanone
US20230255970A1 (en) * 2020-08-12 2023-08-17 The Broad Institute, Inc. Compositions and methods for treating proliferative diseases

Citations (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR1516777A (fr) * 1966-08-02 1968-02-05 Innothera Lab Sa Dérivés du thiazole ainsi que de la thiazolo [4,5-d] pyridazine et leur préparation
FR2270848A1 (ja) * 1974-02-05 1975-12-12 Clin Midy
WO1997015567A1 (de) * 1995-10-20 1997-05-01 Dr. Karl Thomae Gmbh 5-gliedrige heterocyclen, diese verbindungen enthaltende arzneimittel und deren verwendung sowie verfahren zu ihrer herstellung
DE10208256A1 (de) * 2002-02-26 2003-09-04 Bayer Ag Piperidinouracile
EP1352650A1 (en) * 2000-12-18 2003-10-15 Institute of Medicinal Molecular Design, Inc. Inhibitors against the production and release of inflammatory cytokines
WO2004014882A2 (en) * 2002-08-09 2004-02-19 Axys Pharmaceuticals Proteasome inhibitors : peptide derivatives having c-terminal heteroaryl groups
WO2004018453A1 (ja) * 2002-08-23 2004-03-04 Dainippon Pharmaceutical Co., Ltd. プロリン誘導体
WO2004041815A1 (de) * 2002-11-08 2004-05-21 Merck Patent Gmbh Indolderivate mit 5ht1a affinität
WO2004058751A1 (en) * 2002-12-24 2004-07-15 Metris Therapeutics Limited Piperidinyl-thiazole carboxamide derivatives for altering vascular tone
WO2005003128A1 (en) * 2003-06-25 2005-01-13 Merck Patent Gmbh Thiazolylpiperidine derivatives as mtp inhibitors
WO2005058887A1 (en) * 2003-12-08 2005-06-30 F. Hoffmann-La Roche Ag Novel thiazole derivates

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4731446A (en) * 1987-05-01 1988-03-15 The Dow Chemical Company Imidazo[1,2-a]pyrimidine sulfonic acids and acid halides
US5510478A (en) * 1994-11-30 1996-04-23 American Home Products Corporation 2-arylamidothiazole derivatives with CNS activity
CN1063442C (zh) * 1995-05-18 2001-03-21 泽里新药工业株式会社 氨基噻唑衍生物、含有它们的药物组合物及其用途
JPH0987282A (ja) * 1995-09-21 1997-03-31 Kyowa Hakko Kogyo Co Ltd チアゾール誘導体
ATE231137T1 (de) * 1996-10-24 2003-02-15 Zeria Pharm Co Ltd Substituierte benzoylthiazolderivate und sie enthaltende medikamente
ES2198719T3 (es) * 1997-06-24 2004-02-01 Zeria Pharmaceutical Co., Ltd. Procedimiento de produccion de los derivados de 2-hidroxibenzamida.
US6100282A (en) * 1998-01-02 2000-08-08 Hoffman-La Roche Inc. Thiazole derivatives
DE19817459A1 (de) * 1998-04-20 1999-10-21 Basf Ag Neue heterozyklische substituierte Amide, Herstellung und Anwendung
CN1211375C (zh) * 1998-10-22 2005-07-20 弗·哈夫曼-拉罗切有限公司 噻唑衍生物
ES2360933T3 (es) * 2000-04-27 2011-06-10 Astellas Pharma Inc. Derivados de heteroarilo condensados.
WO2002020010A1 (en) * 2000-09-08 2002-03-14 Zeria Pharmaceutical Co., Ltd. Pharmaceutical compositions containing aminothiazole derivatives for the treatment of colonic motor dysfunctions
US20030073836A1 (en) * 2001-07-05 2003-04-17 Boehringer Ingelheim Pharma Kg Heteroarylcarboxylic acid amides, the preparation thereof and their use as pharmaceutical compositions
DE10132686A1 (de) * 2001-07-05 2003-01-16 Boehringer Ingelheim Pharma Heteroarylcarbonsäureamide, ihre Herstellung und ihre Verwendung als Arzneimittel
US7176242B2 (en) * 2001-11-08 2007-02-13 Elan Pharmaceuticals, Inc. N,N′-substituted-1,3-diamino-2-hydroxypropane derivatives
WO2003099316A1 (en) * 2002-05-20 2003-12-04 Bristol-Myers Squibb Company Heterocyclicsulfonamide hepatitis c virus inhibitors
CA2514573A1 (en) * 2003-01-27 2004-08-12 Astellas Pharma Inc. Thiazole derivatives and their use as vap-1 inhibitors
GB0412468D0 (en) * 2004-06-04 2004-07-07 Astrazeneca Ab Chemical compounds
EP1797084A1 (en) * 2004-09-20 2007-06-20 4Sc Ag NOVEL HETEROCYCLIC NF-kB INHIBITORS
KR20080031038A (ko) * 2005-07-29 2008-04-07 4에스체 악티엔게젤샤프트 신규의 헤테로환 ＮＦ-κＢ 억제제
EP1834954A1 (en) * 2006-03-15 2007-09-19 4Sc Ag Thiazoles as NF-kB Inhibitors (proteasome inhibitors)
EP2313435A4 (en) * 2008-07-01 2012-08-08 Aveo Pharmaceuticals Inc FIBROBLAST GROWTH FACTOR RECEPTOR 3 (FGFR3) BINDING PROTEINS

Patent Citations (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR1516777A (fr) * 1966-08-02 1968-02-05 Innothera Lab Sa Dérivés du thiazole ainsi que de la thiazolo [4,5-d] pyridazine et leur préparation
FR2270848A1 (ja) * 1974-02-05 1975-12-12 Clin Midy
WO1997015567A1 (de) * 1995-10-20 1997-05-01 Dr. Karl Thomae Gmbh 5-gliedrige heterocyclen, diese verbindungen enthaltende arzneimittel und deren verwendung sowie verfahren zu ihrer herstellung
EP1352650A1 (en) * 2000-12-18 2003-10-15 Institute of Medicinal Molecular Design, Inc. Inhibitors against the production and release of inflammatory cytokines
DE10208256A1 (de) * 2002-02-26 2003-09-04 Bayer Ag Piperidinouracile
WO2004014882A2 (en) * 2002-08-09 2004-02-19 Axys Pharmaceuticals Proteasome inhibitors : peptide derivatives having c-terminal heteroaryl groups
WO2004018453A1 (ja) * 2002-08-23 2004-03-04 Dainippon Pharmaceutical Co., Ltd. プロリン誘導体
WO2004041815A1 (de) * 2002-11-08 2004-05-21 Merck Patent Gmbh Indolderivate mit 5ht1a affinität
WO2004058751A1 (en) * 2002-12-24 2004-07-15 Metris Therapeutics Limited Piperidinyl-thiazole carboxamide derivatives for altering vascular tone
WO2004058750A1 (en) * 2002-12-24 2004-07-15 Metris Therapeutics Limited Piperidinyl-thiazole carboxylic acid derivatives as angiogenesis inhibitors
WO2005003128A1 (en) * 2003-06-25 2005-01-13 Merck Patent Gmbh Thiazolylpiperidine derivatives as mtp inhibitors
WO2005058887A1 (en) * 2003-12-08 2005-06-30 F. Hoffmann-La Roche Ag Novel thiazole derivates

Non-Patent Citations (15)

* Cited by examiner, † Cited by third party
Title
BOGER D.L. ET AL.: "A new class of highly cytotoxic diketopiperazines", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, OXFORD, GB, vol. 10, no. 10, May 2000 (2000-05), pages 1019-1020, XP004204595, ISSN: 0960-894X, Compounds 6 and 8 *
C. HAHNEMANN, H. HARTMANN: "On the Reaction of Thiazole-2,4-diamines with Isothiocyanates - Preparation and Transformation of 2,4-Diaminothiazol e-5-carbothioamides", HELVETICA CHIMICA ACTA, vol. 86, 2003, pages 1949-1965, XP002346496, Compounds 8a-b,d, 15f, 29e-g, 31a-e, 34a, 35a, 38a, 38d, 39a, 39d *
EKAMBARESWARA RAO K. ET AL.: "Synthesis of Novel Thiazole-Containing DNA Minor Groove Binding Oligopeptides Related to the Antibiotic Distamycin", JOURNAL OF ORGANIC CHEMISTRY, AMERICAN CHEMICAL SOCIETY. EASTON, US, vol. 55, no. 2, 1990, pages 728-737, XP002255609, ISSN: 0022-3263, Compound 30 *
EL-SUBBAGH H. ET AL.: "2,4-Disubstituted thiazoles II. A novel class of anatitumor agents, synthesis and biological evaluation", EUROPEAN JOURNAL OF MEDICAL CHEMISTRY, EDITIONS SCIENTIFIQUE ELSEVIER, PARIS, FR, vol.31, no. 12, 1996, pages 1017-1021, XP004071797, ISSN: 0223-5234, Compunds 7 and 9 *
FRANCHETTI P. ET AL.: "A new C-nucleoside analogue of tiazofurin - synthesis and biological evaluation of 2-beta-d-ribofuranosylimidazole-4-carboxam ide (imidazofurin)", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, OXFORD, GB, vol. 11, no. 1, 8 January 2001 (2001-01-08), pages 67-69, XP004225324, ISSN: 0960-894X, Oxazofurin, Compound 1 *
J. DAS ET AL.: "Thromboxane A2/Endoperoxide Receptor Antagonists: 1,3-Dioxane and 1,3-Dioxolane Analogs", BIOORG. MED. CHEM. LETT., vol. 3, no. 6, 1993, pages 1271-1276, XP002346707, Compounds 1a-1f *
LANGE U.E.W. ET AL.: "Synthesis of Highly potent and Selective Hetaryl Ureas as Integrin avb3-Receptor Antagonists". BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, OXFORD, GB, vol. 12, 2002, pages 1379-1382, XP002289253, ISSN: 0960-894X, Compounds 23a and 25a *
M. HERRMANN ET AL.: "Chemical Modification of Thiangazole A in the Oxazole and Styryl Region", EUROPEAN JOURNAL OF ORGANIC CHEMISTRY, vol. 12, 1999, pages 3381-3392, XP002346499, Compounds 1a-b, 2a-b, 5-11, 17, 21-22, 27-29, 32-33, 35, 36-47, 51-57 *
P. WIPF, S. VENKATRAMAN: "From Aziridines to Oxazolines and Thiazolines: The Heterocyclic Route to Thiangazole", SYNLETT, vol. 1, 1997, pages 1-10, XP002346498, Compounds 85, 87-88, 91, 94-95, 97, 99-100 *
P. WIPF, S. VENKATRAMAN: "Total Synthesis of (-)-Thiangazole and Structurally Related Polyazoles", JOURNAL OF ORGANIC CHEMISTRY, vol. 60, 1995, pages 7224-7229, XP002346495, Tantazoles A-B, F, Didehydrotantazole, Compounds 11, 13-14, 16-17 *
P.-Y. COQUERON ET AL.: "Iterativer Aufbau von Oxazolringen uber alpha-Chlorglycinate: Total synthese von (-)-Muscorid A", ANGEWANDTE CHEMIE, vol. 115, no. 12, 2003, pages 1451-1454, XP002346497, Compound 22 *
R. KUMAR, J. WILLIAM LOWN: "Synthesis and Antitumot Cytotoxicity Evalutation of Novel Thiazole-Containing Glycosylated Polyamides", EUR. J. ORG. CHEM., vol. 24, 2003, pages 4842-4851, XP002346491, Compounds 26-27 *
R.J. BOYCE, G. PATTENDEN: "Naturally Occuring 4-Methylthiazolines. A total Synthesis of (-)-'4R,4S' !-Didehyrdomirabazole A", TETRAHEDRON, vol. 51, no. 26, 1995, pages 7313-7320, XP002346493, Compounds 3, 9 and 13 *
R.L. PARSONS JR., CH. HEATHCOCK: "Total Synthesis of (-)-Thiangazole, a Naturally-Occuring HIV-1 Inhibitor", JOURNAL OF ORGANIC CHEMISTRY, vol. 59, 1994, pages 4733-4734, XP002346494, Compounds 1-2, 12 *
WIPF P. ET AL.: "Total Synthesis of (-)-Muscoride A", JOURNAL OF ORGANIC CHEMISTRY, AMERICAN CHEMICAL SOCIETY, WASHINGTON, DC, US, vol. 61, 1996, pages 6517-6522, XP002199739, ISSN: 0022-3263, Compound 9 *

Also Published As

Publication number Publication date
US8106048B2 (en) 2012-01-31
CN101031567B (zh) 2011-12-21
US20080261971A1 (en) 2008-10-23
EP1797084A1 (en) 2007-06-20
CN101031567A (zh) 2007-09-05
EA200700441A1 (ru) 2007-10-26
CA2580725A1 (en) 2006-03-30
BRPI0516958A (pt) 2008-03-25
AU2005287692B2 (en) 2012-07-12
JP2008513386A (ja) 2008-05-01
NZ553734A (en) 2011-01-28
MX2007003115A (es) 2007-07-16
AU2005287692A1 (en) 2006-03-30
WO2006032322A1 (en) 2006-03-30

Similar Documents

Publication Publication Date Title
EA012607B1 (ru) НОВЫЕ ГЕТЕРОЦИКЛИЧЕСКИЕ ИНГИБИТОРЫ NF-κB
US7812041B2 (en) Heterocyclic NF-κB inhibitors
TWI461423B (zh) 用於治療Pim激酶相關病狀及疾病之噻唑啶二酮化合物
US8088806B2 (en) Thiazole compounds and methods of use
US7087614B2 (en) Pyrimidine inhibitors of phosphodiesterase (PDE) 7
KR101804588B1 (ko) 조혈 성장 인자 모방체 소분자 화합물 및 이의 용도
EA016300B1 (ru) НОВЫЕ ГЕТЕРОЦИКЛИЧЕСКИЕ ИНГИБИТОРЫ NF-κB
JP6117430B2 (ja) 選択的ヒストン脱アセチル化酵素抑制剤としての新規化合物およびこれを含む薬剤学的組成物
JP5517935B2 (ja) 細胞壊死阻害剤としてのインドール及びインダゾール化合物
US20100048574A1 (en) NOVEL HETEROCYCLIC NF-kB INHIBITORS
KR20010085984A (ko) 2-우레이도-티아졸 유도체, 이의 제조방법 및항암제로서의 이의 용도
US20100292266A1 (en) Oxazolyl Piperidine Modulators of Fatty Acid Amide Hydrolase
AU2007207055A1 (en) Thiazoles as 11 beta-HSD1 inhibitors
JP2020503268A (ja) 選択的ｈｄａｃ１、２阻害剤としてのピペラジン誘導体
KR20080012304A (ko) 피라졸 화합물 및 이들 피라졸 화합물을 포함하여이루어지는 당뇨병 치료약
EA009882B1 (ru) Замещенные арилацилтиомочевины и родственные соединения; ингибиторы репликации вирусов
CN111315734B (zh) 作为食欲素受体拮抗剂的经取代的2-氮杂双环[3.1.1]庚烷和2-氮杂双环[3.2.1]辛烷衍生物
KR101457339B1 (ko) 아랄킬 치환된 피페리딘 또는 피페라진 유도체 및 정신분열증 치료를 위한 이의 용도
CN101646460A (zh) 含有具有组蛋白脱乙酰化酶抑制作用的化合物作为有效成分的降眼压剂
CA2503713A1 (en) Piperidinyl cyclopentyl aryl benzylamide modulators of chemokine receptor activity
KR20110120878A (ko) 치환된 퀴나졸린 화합물
KR20120013266A (ko) 세포괴사 저해제로서의 인돌 및 인다졸 화합물
KR20080104147A (ko) 신규의 헤테로환 ＮＦ-κＢ 억제제
JP3348505B2 (ja) ベンゾオキサジン−３−オン化合物
US20110034466A1 (en) Novel five-membered ring compound

Legal Events

Date Code Title Description
MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ BY KZ KG MD TJ TM RU